PF-04418948 inhibited prostaglandin E(2)(PGE(2))-induced increase in cAMP in cells expressing EP(2) receptors with a functional K(B) value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent K(B) of 5.4 nM. In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE(2)-induced relaxation curve with a K(B) of 2.5 nM and an apparent K(B) of 1.3 nM respectively. Reversal of the PGE(2)-induced relaxation in the mouse trachea by PF-04418948 produced an IC(50) value of 2.7 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 50 mg/mL|
Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor.
Birrell MA, et al. Br J Pharmacol. 2013 Jan;168(1):129-38. PMID: 22747912.
In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist.
af Forselles KJ, et al. Br J Pharmacol. 2011 Dec;164(7):1847-56. PMID: 21595651.
|Related Prostaglandin Receptor Products|
Dinoprost tromethamine (Prostaglandin F2α tromethamine) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist.
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM.
Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.
GW627368X is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity.
Taprenepag, also known as CP-544326, is a potent and selective EP(2) receptor agonist, with IC50 values of 10 and 15 nM for human and rat EP2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.